癌症预防剂，第2部分：2-苯基-4-喹诺酮和9-氧代-9,10-二氢吖啶衍生物作为新型抗肿瘤促进剂的合成与评价

Cancer preventive agents, Part 2: Synthesis and evaluation of 2-phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives as novel antitumor promoters.

作者信息

Nakamura Seikou, Kozuka Mutsuo, Bastow Kenneth F, Tokuda Harukuni, Nishino Hoyoku, Suzuki Madoka, Tatsuzaki Jin, Morris Natschke Susan L, Kuo Sheng-Chu, Lee Kuo-Hsiung

机构信息

Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.

出版信息

Bioorg Med Chem. 2005 Jul 15;13(14):4396-401. doi: 10.1016/j.bmc.2005.04.078.

DOI:10.1016/j.bmc.2005.04.078

PMID:15914009

Abstract

2-Phenyl-4-quinolone and 9-oxo-9,10-dihydroacridine derivatives were synthesized and screened as potential antitumor promoters by examining the ability of the compounds to inhibit Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Interestingly, compounds 14, 15, and 17 showed similar inhibitory effects (89-92%, 66-69%, and 24-29% at 1000, 500, and 100 mol ratio to TPA, respectively) against EBV-EA with potencies comparable to those of glycyrrhetic acid, a known natural antitumor-promoter.

摘要

合成了2-苯基-4-喹诺酮和9-氧代-9,10-二氢吖啶衍生物，并通过检测这些化合物抑制肿瘤启动子12-O-十四烷酰佛波醇-13-乙酸酯（TPA）在Raji细胞中诱导的爱泼斯坦-巴尔病毒早期抗原（EBV-EA）激活的能力，将其作为潜在的抗肿瘤启动子进行筛选。有趣的是，化合物14、15和17对EBV-EA显示出相似的抑制作用（与TPA的摩尔比分别为1000、500和100时，抑制率分别为89-92%、66-69%和24-29%），其效力与已知的天然抗肿瘤启动子甘草次酸相当。